Abstract:
:Berberine was investigated as an inhibitor of human protein tyrosine phosphatase 1B (h-PTP 1B) in an attempt to explain its anti-hyperglycemic activitiy. The investigation included simulated docking experiments to fit berberine within the binding pocket of h-PTP 1B. Berberine was found to readily fit within the binding pocket of h-PTP 1B in a low energy orientation characterized with optimal electrostatic attractive interactions bridging the isoquinolinium positively charged nitrogen atom of berberine and the negatively charged acidic residue of ASP 48 of h-PTP 1B. Experimentally, berberine was found to potently competitively inhibit recombinant h-PTP 1B in vitro (Ki value = 91.3 nM). Our findings strongly suggest that h-PTP 1B inhibition is at least one of the reasons for the reported anti-hyperglycemic activities of berberine.
journal_name
J Enzyme Inhib Med Chemjournal_title
Journal of enzyme inhibition and medicinal chemistryauthors
Bustanji Y,Taha MO,Yousef AM,Al-Bakri AGdoi
10.1080/14756360500533026subject
Has Abstractpub_date
2006-04-01 00:00:00pages
163-71issue
2eissn
1475-6366issn
1475-6374journal_volume
21pub_type
杂志文章abstract::HGF/c-Met signalling pathway plays an important role in the development of cancers. A series of 6,7-dimethoxy-4-anilinoquinolines possessing benzimidazole moiety were synthesised and identified as potent inhibitors of the tyrosine kinase c-Met. Their in vitro biological activities against three cancer cell lines (A549...
journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章,评审
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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更新日期:2013-02-01 00:00:00
abstract:UNLABELLED:Context: Garcinia hombroniana Pierre, known as manggis hutan in Malaysia is a rich source of xanthones and benzophenones. OBJECTIVES:This study was aimed to isolate and characterize potential cholinesterase inhibitors from the extracts of G. hombroniana bark and investigate their interactions with the enzym...
journal_title:Journal of enzyme inhibition and medicinal chemistry
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更新日期:2015-02-01 00:00:00
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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更新日期:2013-06-01 00:00:00
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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abstract::Histone demethylation is a vital process in epigenetic regulation of gene expression. A number of histone demethylases are present to control the methylated states of histone. Among these enzymes, KDM4s are one subfamily of JmjC KDMs and play important roles in both normal and cancer cells. The discovery of KDM4s inhi...
journal_title:Journal of enzyme inhibition and medicinal chemistry
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abstract::An efficient and simple microwave assisted synthesis of sulfonamide derivatives incorporating the pyridazine moiety has been developed. These sulfonamides were used for the preparation of new heterocyclic compounds via reaction with different reagents using a microwave irradiation technique. The structures of the newl...
journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
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更新日期:2013-12-01 00:00:00
abstract::In mammalian skin, melanocyte proliferation and melanogenesis can be stimulated by keratinocytes, fibroblasts and other regulatory factors. To determine whether hydroxybenzyl alcohols (HBAs) show more inhibitory in melanocytes cultured alone or in melanocytes co-cultured with keratinocytes, we developed a murine melan...
journal_title:Journal of enzyme inhibition and medicinal chemistry
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abstract::The reaction mechanism of glycoside hydrolases belonging to family 1 (GH1) of carbohydrate-active enzymes classification, hydrolysing β-O-glycosidic bonds, is well characterised. This family includes several thousands of enzymes with more than 20 different EC numbers depending on the sugar glycone recognised as substr...
journal_title:Journal of enzyme inhibition and medicinal chemistry
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更新日期:2019-12-01 00:00:00
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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更新日期:2020-12-01 00:00:00
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journal_title:Journal of enzyme inhibition and medicinal chemistry
pub_type: 杂志文章
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更新日期:2015-06-01 00:00:00
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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更新日期:2018-12-01 00:00:00
abstract::Fatty acid synthase (FAS) has been proposed to be a new drug target for the development of anticancer agents because of the significant difference in expression of FAS between normal and tumour cells. Since a n-hexane-soluble extract from Ginkgo biloba was demonstrated to inhibit FAS activity in our preliminary test, ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
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doi:10.3109/14756366.2012.658786
更新日期:2013-06-01 00:00:00
abstract::Exposure of the N-methoxycarbonyl-bicyclic-keto-acid 5 (improved preparation) to the Barnick beta-keto-acid synthesis yielded an aqueous solution of the sodium salts of the beta-keto-acids 26 and 27 which on heating at 60-65 degrees C furnished the N-methoxycarbonyl-tricyclic-ketone 9 (55%) plus the hydroxy-ketone 28 ...
journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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更新日期:2011-08-01 00:00:00
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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更新日期:2016-08-01 00:00:00
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journal_title:Journal of enzyme inhibition and medicinal chemistry
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abstract::The inhibition of two human carbonic anhydrase (HCA, EC 4.2.1.1) isozymes, the cytosolic HCA I and II, with heavy metal salts of Pb(II), Co(II) and Hg(II) has been investigated. Human erythrocyte CA-I isozyme was purified with a specific activity of 920 EUmg(-1) and a yield of 30% and CA-II isozyme was purified with a...
journal_title:Journal of enzyme inhibition and medicinal chemistry
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abstract::The antioxidant properties and inhibitory effect on early tumor promoter markers of A. marmelos (25 and 50 mg/Kg b. wt. orally) have been evaluated. Male Wistar rats were pre-treated for seven consecutive days with A. marmelos prior to CCl4 (1 mL Kg(- 1) body weight p. o., in corn oil [1:1 v/v]) treatment. Pre-treatme...
journal_title:Journal of enzyme inhibition and medicinal chemistry
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